Succinate dehydrogenase (SDH) has been identified as an important target fungicide discovery and the SDH inhibitor (SDHI) displayed a broad-spectrum activity against various fungal species. The report from Phillips McDougall showed that the global market of SDHI fungicides would reach up to US $3.4 billion by 2026. Therefore, the discovery of novel SDHI is a very hot area in pesticide discovery.<br/>Pydiflumetofen bearing a novel amide bond linker, developed by Syngenta, is an ultra-high activity and wide-spectrum fungicide. However, the high persistence of pydiflumetofen in soil both in laboratory and field limits its further development. In order to improve its metabolism property, based on the interaction of pydiflumetofen-SDH, the receptor-based scaffold hopping method was designed to optimize the methyl (colored by blue) and phenethyl (colored by red) in pydiflumetofen (Figure 1). After substituent optimization, compound Y19315 was successfully identified with good inhibitory activity against many plant pathogens. Most importantly, the double bond linked with benzene ring in Y19315 gives it good metabolic properties compared to pydiflumetofen.

Discovery of succinate dehydrogenase fungicide via receptor-based scaffold-hopping

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ACS Fall 2022

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